Hoffmann-la Roche Inc.

Peter Vogt

Michelangelo Scalone

Markus Hohler

Henri Ramuz

Jean-Claude Muller

Bruno Lohri

Marquard Imfeld

A process is disclosed for the manufacture of amides, including peptides, in which a carboxylic acid is reacted with a primary or secondary amine in the presence of a carbodiimide and a catalytic amount of N-hydroxy compound.

Process for producing amides using catalytic amounts of an N-hydroxy

The present invention is concerned with a novel process for the making of a compound of formula I ##STR1## by oxidizing the corresponding 3-hydroxymethyl-cephem derivative with an inorganic hypohalite or inorganic halite in the presence of compounds of formula III ##STR2## is wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and Y are as defined herein. The process is useful for providing 3-formyl-cephem compounds useful in the making of cephalosporin derivatives.

Process for making 3-formylcephem derivatives

A process for the manufacture of amides, including peptides, by reacting a carboxylic acid with a primary or secondary amine in the presence of a carbodiimide and a catalytic amount of a N-hydroxy compound.

It has been found that pyridine-2-carboxamides of the formula ##STR1## wherein R is amino or a residue convertible into amino, and pharmaceutically usable acid addition salts of that carboxamide in which R is amino can be prepared in a simple manner and in good yield by reacting 2,5-dichloropyridine in the presence of a palladium-phosphine catalyst with an alkyne of the formula

Process for preparing pyridine-2-carboxamides

Process for preparing pyridine 2-carboxamides

Novel pyrimidinedicarbamates of the formula ##STR1## wherein R is lower alkyl or (lower alkyloxy)-(lower alkyl) and X is a leaving group, can be manufactured by carbamoylating the corresponding free diamines. They are valuable intermediates and can be used, for example, for the manufacture of corresponding oxadiazolopyrimidines of the formula ##STR2## and pharmaceutically acceptable salts thereof. The latter have valuable long-lasting vasodilating and/or bloodpressure lowering properties and are accordingly suitable especially for the treatment of vascular-conditioned hypertensions or as vasodilators in the case of peripheral blood supply disorders.

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Birsfelden, Switzerland

Peter Vogt